JPH07215830A - Composition for oral cavity - Google Patents

Abstract

PURPOSE:To obtain the subject composition prevented from decline in its antibacterial activity by incorporating cetyl pyridinium chloride with a specific surfactant. CONSTITUTION:This composition for oral cavity is obtained by incorporating cetyl pyridinium chloride with a specific surfactant which is either (1) a fatty acid diethanolamide or (2) a polyethylene glycol fatty acid monoester with the average polymerization degree of 30-55 of the constituent ethylene oxide and/or a polyoxyethylene hardened castor oil with the average polymerization degree of 90-120 of the constituent ethylene oxide.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an oral composition, and more particularly to an oral composition in which the antibacterial effect of cetylpyridinium chloride, which is an antibacterial agent, is prevented from being lowered by a surfactant.

[0002]

BACKGROUND OF THE INVENTION In order to prevent gingivitis, alveolar pyorrhea, and caries, it is important to suppress the formation of plaque. One of them is to prevent chemical plaque formation by quaternary ammonium salts such as cetylpyridinium chloride. Studies on formation inhibition have been conducted. In particular, cetylpyridinium chloride has an antibacterial effect,
Since it is relatively easily adsorbed on the oral mucosa and the tooth surface, it is considered to prevent the adsorption of bacteria on the tooth surface and thus the formation of plaque.

However, cetylpyridinium chloride is highly reactive and forms a salt when an anionic substance such as sodium carboxymethyl cellulose used as a binder for oral compositions and sodium lauryl sulfate commonly used as a foaming agent is added. However, the antibacterial activity is often lost. The cause of inactivation is not only the formation of salts but also the incorporation of surfactants into micelles. However, it is essential to add a sweetener, a flavoring agent, etc. to the oral composition in order to provide ease of use, and particularly when the flavoring agent itself is lipophilic, it is solubilized in the oral composition. Therefore, a surfactant is required. Therefore, it is necessary to select and set the concentration of a surfactant that does not impair the tooth adsorption and antibacterial activity of cetylpyridinium chloride. However, the present situation is that the oral composition has not been sufficiently studied so that the antibacterial activity of cetylpyridinium chloride is not impaired and the transparency, which is a characteristic of the oral composition, can be maintained.

[0004]

DISCLOSURE OF INVENTION Problems to be Solved by the Invention The present inventors conducted a study for the purpose of maintaining the antibacterial activity of cetylpyridinium chloride and preventing the formation of dental plaque. As a result, a specific surfactant was added. By doing so, it was found that the antibacterial effect of cetylpyridinium chloride was hardly reduced, and the present invention was completed.

[0005]

That is, the present invention has achieved the above object by the following means. (1) An oral composition comprising cetylpyridinium chloride and fatty acid diethanolamide. (2) Polyethylene glycol fatty acid monoester having an average degree of polymerization of cetylpyridinium chloride and ethylene oxide of 30 to 55 and / or an average degree of polymerization of 90 to 1
A composition for oral cavity, which comprises 20 of polyoxyethylene hydrogenated castor oil.

[0006] In the present invention, cetylpyridinium chloride (hereinafter referred to as CPC) has a concentration of 0.
The amount is 002% by weight or more, preferably 0.01% by weight or more. From the viewpoint of antibacterial effect, the upper limit of the amount of CPC blended is not particularly limited, but it is not preferable to blend a too large amount in view of the bitterness of CPC and the possibility that teeth may be colored when the amount is large. .

As the fatty acid of the fatty acid diethanolamide of the present invention, a linear fatty acid having 12 or more carbon atoms, for example,
Lauric acid (C12), myristic acid (C1)
4), palmitic acid (16 carbon atoms), stearic acid (18 carbon atoms), or the like, or fatty acids obtained by hydrolyzing these diglycerides or triglycerides, that is, coconut oil fatty acids, etc., and these fatty acids and diethanolamine It is obtained by dehydration condensation of and. In particular, coconut oil fatty acid diethanolamide obtained by condensation of coconut oil fatty acid and diethanolamine is most preferable as the fatty acid diethanolamide of the present invention.
This coconut oil fatty acid and diethanolamine are replaced with lauric acid, stearic acid, etc.
It is produced by using monoethanolamine, isopropanolamine, triethanolamine, etc. instead of diethanolamine, and is divided into 1: 1 type and 1: 2 type according to the reaction ratio of fatty acid and alkylolamine. Can use a mixture of 1: 1 coconut oil fatty acid diethanolamide and lauric acid diethanolamide.

The polyethylene glycol fatty acid monoester has an average degree of polymerization of ethylene oxide of 30.
To polyethylene glycol (40) monostearate, which is 40 to 55, preferably 40. As the polyoxyethylene hydrogenated castor oil, those having an average degree of polymerization of ethylene oxide of 90 to 120, particularly 10
Around 0 is preferable.

The amount of these surfactants to be added to the oral composition of the present invention is about 0.0 based on the composition.
It is 1 to 5% by weight (hereinafter,% means% by weight), preferably 0.05 to 3%. The blending amount in this case varies depending on factors such as the blending amount of a lipophilic substance such as a fragrance and the foamability of the oral composition. Further, since the commercially available surfactant is a polymer, it is sold under the name of the component with the most components in its composition, and because it is not composed of only a single compound, The blending amount is slightly different.

From the viewpoint of the bactericidal action of CPC and the improvement of adsorption to teeth, it is desirable that the pH of the oral composition of the present invention is 5.0 to 8.5. Therefore, the composition for oral cavity can be prepared with monosodium phosphate, disodium phosphate, sodium citrate, citric acid, glucono delta lactone, sodium gluconate or sodium acetate, and hydrates thereof.

The oral composition of the present invention can be prepared into an oral composition such as a concentrated or straight type mouthwash, liquid toothpaste, mouthwash, toothpaste treatment, toothpaste, etc. by the conventional method. The additive is not particularly limited and is not limited to the antibacterial activity of CPC, and is an additive used in a preparation of this type, for example, an abrasive, a binder, a thickener, a foaming agent, a wetting agent, a sweetener, a flavoring agent. Although a preservative can be used, when a foaming agent or a solubilizer is used, an anionic substance that may form a salt with CPC or a polyoxyethylene sorbitan fatty acid ester that may be incorporated into a surfactant micelle is not used. Not preferable.

The components of these agents include geraniol modified alcohol, acetylated sucrose modified alcohol, phenylethyl alcohol modified alcohol, brucine modified alcohol, linalool modified alcohol, diethylphthalate modified alcohol, linalyl acetate modified alcohol, benzyl acetate modified. Alcohol, 10%
Denatonium benzoate Alcohol solution denatured alcohol,
No. 14 denatured alcohol, sodium N-acyl-L-glutamate, ascorbic acid, allantoinchlorohydroxyaluminum, sodium alginate, aloe extract, benzoic acid, sodium benzoate, titanium mica, ethanol, ethylenediaminetetrapolyoxyethylene polyoxypropylene, zinc chloride , Sodium chloride, alkyldiaminoethylglycine hydrochloride solution, chlorhexidine hydrochloride, pyridoxine hydrochloride, eugenol, augon extract, γ-oryzanol, kaolin, brown algae extract, carrageenan, carboxyvinyl polymer, hydrous amorphous silicon oxide, licorice extract, dried aluminum hydroxide Gel, agar, dilute hydrochloric acid, xylitol, xanthan gum, guaizulene, citric acid, sodium citrate, glycerin, glycyrrhizi Acid, dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, beta-
Glycyrrhetinic acid, chlorhexidine gluconate solution, sunflower, magnesium aluminum silicate, sodium silicate, light calcium carbonate, cinnamic alcohol, cinnamic aldehyde, crystalline cellulose, synthetic sodium magnesium silicate, wheat germ oil, saccharin, saccharin sodium, salicylic acid Methyl, aluminum oxide,
Titanium oxide, shikon extract, ground calcium carbonate, tartaric acid, distilled peppermint water, aluminum hydroxide, sodium hydroxide, N-stearoyl-L-glutamate sodium, stevia extract, spearmint oil, purified water, sage extract, sodium cetyl sulfate, soap. Substrate, gelatin, sodium fibrin glycolate, sorbit, sorbit solution, potassium sorbate, talc, sodium hydrogen carbonate, thymol, sodium dehydroacetate, sodium copper chlorophyllin, sodium lactate solution, lactose, concentrated glycerin, white sugar, peppermint oil, Calcium hydrogen phosphate for toothpaste, isobutyl paraoxybenzoate, isopropyl paraoxybenzoate, ethyl paraoxybenzoate, butyl paraoxybenzoate, propyl paraoxybenzoate, methyl paraoxybenzoate Hydroxyethyl cellulose,
Calcium pyrophosphate, glucose, propanol, propylene glycol, bentonite, sodium polyacrylate, polyethylene glycol 300, polyethylene glycol 400, polyethylene glycol 1500,
Polyethylene glycol 6000, polyoxyethylene stearyl ether, polyoxyethylene cetyl ether, polyoxyethylene (200) polyoxypropylene glycol (70), polyvinylpyrrolidone, sodium polyphosphate, d-borneol, microcrystalline wax, maltitol, maltitol Liquid, beeswax, anhydrous ethanol, anhydrous citric acid, anhydrous silicic acid, anhydrous aluminum silicate, anhydrous sodium pyrophosphate, methyl cellulose, 1-menthol, d1-menthol, eucalyptus oil, liquid paraffin, sodium monohydrogen phosphate,
Examples thereof include sodium dihydrogen phosphate, trisodium phosphate, calcium hydrogen phosphate, magnesium phosphate, fragrances and pigments. Also, in lozenges, coating agents, mouthwashes, mouth-cooling agents, chewing gums, drinks, candy, etc., the components are appropriately blended according to the properties of the product.

In the present invention, in addition to CPC, dextranase, lytic enzyme (lysozyme chloride, etc.), mutanase, sorbic acid, alexidine, hinokitiol, alkylglycine, alkyldiaminoethylglycine salt, allantoin, azulene, vitamin E, an active ingredient such as sodium monofluorophosphate, sodium fluoride, cuprous fluoride, and a water-soluble primary or secondary phosphate can be blended. And as herbal medicine, sweet cherry, laurel, ryeok, pea, cashew,
Extracts, dried, etc. A thing can be used.

[0014]

The composition for oral cavity of the present invention is the CPC as described above.
Even when (a) is used in combination with (mixed with) a specific surfactant, no reduction in antibacterial activity due to the surfactant is observed, and there is no practical problem in terms of irritation and taste.

[0015]

EXAMPLES The present invention will be described in more detail below with reference to test examples and experimental examples, but the present invention is not limited thereto. As a test example, a mixed solution of CPC and various surfactants was prepared, and the bactericidal activity of the mixed solution was measured by the method described below.

Test Example Preparation of mixed solution: Each mixed solution was added with the surfactant shown in Table 1 to the test solution in an amount of 0.2% by weight (hereinafter,% means% by weight). 0.5 g of CPC, 50 g of glycerin, and 1 sodium phosphate (dihydrate) in 1 l of the test solution
00 mg, disodium phosphate (12 hydrate) 400 m
g, 30 mg of sodium saccharin, 220 mg of sodium fluoride, 2 g of each surfactant was added to an aqueous solution prepared between pH 6.0 and 6.5 to prepare each mixed solution, which was left for about 1 day and used for each test. . As a control, a product to which no surfactant was added was used. Then, the following was used as the added surfactant. POE means polyoxyethylene.

POE (40) monostearate (MYS
-40) (Nikko Chemicals Co., Ltd.) POE (100) hydrogenated castor oil (HCO-100)
(Nikko Chemicals Co., Ltd.) Coconut oil fatty acid diethanolamide (STAHOME DF-
2) (manufactured by NOF CORPORATION) POE (25) monostearate (MYS-25)
(Nikko Chemicals Co., Ltd.) POE (9) lauryl ether (BL-9EX)
(Nikko Chemicals Co., Ltd.) POE (15) cetyl ether (BC-15TX)
(Manufactured by Nikko Chemicals Co., Ltd.) POE (60) sorbit tetraoleate (GO-4)
60) (manufactured by Nikko Chemicals Co., Ltd.) POE Lanolin (TW-30)
(Manufactured by Nikko Chemicals Co., Ltd.) Decaglyceryl monolaurate (Decaglyn 1)
-L) (Nikko Chemicals Co., Ltd.)

Bactericidal test: A viable suspension of Streptococcus myutans MT8148R (about 1 × 10 ⁸ ce) precultured in a BHI (Difco) liquid medium.
(11 / ml) (100 μl) was added to each mixed solution (400 μl) and immediately stirred with a vortex mixer. Exactly 10 seconds after adding the viable cell suspension, 100 μl of this S
The mixture was added to CDLP medium (manufactured by Nippon Pharmaceutical Co., Ltd.) and diluted 100 times. Next, add 1 ml of this to 0.7% Twin 80 (Twee
n80) -added BHI agar medium (agar 1.0%) was poured into a Petri dish, mixed and solidified, and cultured at 36 ° C. for 48 hours. Then, the number of colonies appearing on the BHI agar medium was counted. Further, the same operation was performed on a control solution containing no surfactant, and the degree of inhibition of the CPC antibacterial activity of the surfactant was calculated by the following formula (1). The results were calculated by averaging three petri dishes, and the results are shown in Table 1.

Formula (1) Degree of inhibition of antibacterial activity of CPC by surfactant = log
(Bs / Bcpc) (Bs in the formula represents the viable cell count per 1 ml immediately after contacting the CPC-containing surfactant-added formulation with the bacterial solution for 10 seconds, and Bcpc is the CPC-containing formulation containing no surfactant. Indicates the viable cell count when the bacterial solution was contacted in the same manner.)

In this formula, the calculated numerical value shows the antibacterial activity of CPC by the addition of the surfactant, and the degree of inhibition is 0.
If the value is less than 0, the addition of the surfactant has no effect. If it is less than 0, the antibacterial activity of CPC is increased, and if it is greater than 0, the antibacterial activity of CPC is decreased.

[0021]

[Table 1]

[0022]

[0023]

[0024]

[0025]

[0026]

[0027]

[0028]

INDUSTRIAL APPLICABILITY According to the present invention, by using (mixing) CPC together with a specific surfactant, CPC by the surfactant can be obtained.
The bactericidal effect is not reduced, and there is no practical problem in terms of irritation and taste, and a sufficient effect as an oral composition is obtained.

Claims (2)

[Claims] 1. An oral composition comprising cetylpyridinium chloride and fatty acid diethanolamide. 2. A polyethylene glycol fatty acid monoester having an average degree of polymerization of cetylpyridinium chloride and ethylene oxide of 30 to 55 and / or a polyoxyethylene hydrogenated castor oil having an average degree of polymerization of ethylene oxide of 90 to 120 are blended. A composition for oral cavity characterized by the above.